Formulation Development and Characterization of Floating Drug Delivery System of Rosiglitazone Maleate

Alagusundaram M, P. Keshri, M. Tyagi, N. Jain, G. Venkateshwarlu, D. Gupta
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Abstract

In the current study, wet granulation with various concentrations and combinations of excipients like magnesium stearate as a lubricant, talc as glident, DCP as diluent, and PVP K 30 as a binder successfully produced floating tablets of rosiglitazone maleate. These excipients included HPMC K15M, xanthan gum, sodium bicarbonate, and tartaric acid as gas-generating agents. We investigated every pre-compressional parameter, including angle of repose, bulk density, and Carr's index. Drug content, hardness, friability, weight fluctuation, in-vitro dissolving experiments, floating qualities, and stability investigations were performed on the compressed tablets. According to in-vitro experiments, the release time increases up to 6, 8, and 10 hours, respectively, as the content of HPMC K15M in formulations F1, F2, and F3 is raised. For formulations F4, F5, and F6, adding xanthan gum raised the release to 7, 9, and 11 hours, respectively. In formulations F7, F8, and F9, the release was found to be increased up to 8, 10, and 12 hours, respectively, with the addition of HPMC K 15 M and Xanthan gum. F9 was discovered to be the finest formulation since it could maintain release for up to 12 hours. All formulations displayed "n" value for Peppa's plot in the range of 0.45 to 0.89, demonstrating anomalous transport (non-Fickian diffusion) as the method of drug release. The improved formulation (F9) was demonstrated to be stable and intact without any contact over the course of 90 days.
马来酸罗格列酮漂浮给药体系的研制与表征
在本研究中,采用硬脂酸镁作为润滑剂、滑石粉作为润滑剂、DCP作为稀释剂、PVP k30作为粘合剂等不同浓度和组合的辅料湿造粒,成功生产出马来酸罗格列酮漂浮片。这些赋形剂包括HPMC K15M、黄原胶、碳酸氢钠和酒石酸作为气体生成剂。我们研究了每一个压缩前参数,包括休止角、体积密度和卡尔指数。对该压缩片进行了药物含量、硬度、脆性、重量波动、体外溶出实验、漂浮质量和稳定性研究。体外实验表明,随着配方F1、F2、F3中HPMC K15M含量的增加,释放时间分别延长至6、8、10小时。对于配方F4, F5和F6,添加黄原胶分别将释放时间提高到7,9和11小时。在配方F7、F8和F9中,添加HPMC k15m和黄原胶后,释放量分别增加到8、10和12小时。F9被发现是最好的配方,因为它可以保持释放长达12小时。所有配方中Peppa图的“n”值均在0.45 ~ 0.89范围内,说明药物释放方式为异常转运(非菲克扩散)。改良后的配方(F9)在90天内被证明是稳定和完整的,没有任何接触。
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